作者: Eric C. Hosten , Felix Odame , Felix Odame , Carminita Frost , Jason Krause
DOI: 10.1007/S00044-021-02706-9
关键词: Stereochemistry 、 Pharmacology toxicology 、 Breast cancer cells 、 Cytotoxicity 、 Cell culture 、 Chemistry 、 Cell cycle checkpoint 、 Crystal structure
摘要: Various benzoxazepine derivatives have been synthesized and characterized using IR, NMR, GC–MS, microanalysis. The single-crystal X-ray structures of 2,2-dimethyl-4-[(E)-2-(4-methylphenyl)ethenyl]-2,3-dihydro-1,5-benzoxazepine (RS01), 4-[(E)-2-(2-chlorophenyl)ethenyl] -2,2-dimethyl-2,3-dihydro-1,5-benzoxazepine (RS05), 2,2,4-trimethyl-2,3-dihydrobenzothiazepine (RS11), 2,2,4-trimethyl-2,3-dihydrobenzoxazepine (RS12) discussed. compounds evaluated for their anticancer properties in breast cancer cells. 4-[(E)-2-(2-Chlorophenyl)ethenyl]-2,2-dimethyl-2,3-dihydro-1,5-benzoxazepine (RS03) RS12 displayed potent cytotoxicity both benign (MCF-7) metastatic (MDA-MB-231) These were more selective the MCF-7 cells with RS03 being most compound (IC50 = 15 µM) series. Upon further investigation, it was found that induced cell cycle arrest G2/M phase display limited toxicity against noncancerous line, MCF-10A.